1 kits (10 Vials)
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Menene Dermorphin?
Dermorphin shine na halitta heptapeptide μ-opioid agonist (MOR) agonist tare da m analgesic effects. Dermorphin shine peptide na opioid na endogenous. A matsayin peptide na bioactive tare da tasirin analgesic mai ƙarfi, yana zaɓin ɗaure ga masu karɓar μ-opioid tare da babban alaƙa, yana nuna ƙarfin analgesic fiye da morphine. Baya ga abubuwan analgesic ɗin sa, Dermorphin kuma yana yin wasu tasirin ilimin lissafi, kamar daidaitawar numfashi, ayyukan zuciya da jijiyoyin jini, da shiga cikin tsarin neuroendocrine. Saboda ingantaccen halayen analgesic, yana da mahimmanci a fagen bincike na ciwo, yana ba da haske da maƙasudi don haɓaka sabbin magungunan analgesic.
▎ Binciken Dermorphin
Menene asalin bincike na Dermorphin?
Binciken Abubuwan Halittu: Tun daga shekarun 1970s, masana kimiyya sun sadaukar da kansu don nemo abubuwa tare da ayyukan ilimin lissafi na musamman daga rayayyun halittu. A hankali mutane sun gane cewa a cikin dogon tsarin juyin halitta, dabbobi za su samar da nau'ikan kwayoyin halitta daban-daban don dacewa da muhalli da kuma kula da ayyukan rayuwa, kuma waɗannan kwayoyin suna iya samun mahimman dabi'un magani.
Musamman Fatar Amphibian: Fatar masu amphibians tana da ayyuka da yawa, kamar numfashi, kariya, da ɓoyewa. Glandar fata na amphibians na iya ɓoye adadi mai yawa na abubuwa masu rai, waɗanda ke taka muhimmiyar rawa wajen karewa daga maƙiyan halitta da daidaitawa ga yanayin. Sirrin fata na yawancin masu amphibians sun ƙunshi abubuwa masu yawa na peptide, waɗanda ke da tsari daban-daban da kuma ayyukan nazarin halittu daban-daban, suna jawo hankalin masana kimiyya da yawa.
Gano Dermorphin: A cikin 1981, masana kimiyya na Italiya sun fara ware Dermorphin daga ɓoyewar fata na kudan itacen Kudancin Amurka (Phyllomedusa sauvagii). Ta hanyar nazarin abubuwan da ke tattare da sirrin fata na bishiyar bishiyar da kuma gano ayyukan nazarin halittu, an gano cewa Dermorphin a ciki yana da tasirin analgesic mai ƙarfi da kuma kusanci ga masu karɓar opioid. Wannan binciken ya buɗe sabon jagorar bincike a fagen maganin ciwo.
Menene tsarin aikin Dermorphin?
1. Daure ga Masu karɓar Opioid
Dermorphin shine peptide mai ƙarfi-kamar opioid wanda zai iya zaɓin ɗaure ga masu karɓar μ-opioid. Wannan ɗaurin yana kunna masu karɓa, yana haifar da jerin tasirin ilimin lissafi [1, 2] . Misali, a cikin gwaje-gwajen dabba, ya nuna tasirin analgesic mai ƙarfi [1, 2] . Ana iya samun sakamako na analgesic ta hanyar hana watsa siginar zafi. Lokacin da aka watsa siginar jin zafi zuwa ƙwayoyin cuta, zai haifar da tashin hankali da harbe-harbe na neurons. Bayan Dermorphin ya ɗaure ga mai karɓar μ-opioid, zai iya hana tashin hankali na neurons, ta haka ne ya rage watsa siginar zafi.
2. Tasiri akan Tsarin Jijiya
Tasiri a Matsayin Igiyar Spinal
A cikin nazarin ɗan adam, an gano cewa jiko na dermorphin na cikin jini na iya haifar da haɓaka mai mahimmanci da ci gaba a cikin ƙofa na flexor reflex na nociceptive a cikin masu sa kai masu lafiya [2] . Wannan yana nuna cewa dermorphin zai iya hana watsa siginar nociceptive a matakin kashin baya. Har ila yau, wannan tasirin yana bayyana a cikin batutuwa masu cikakken rauni na kashin baya, yana kara tabbatar da cewa dermorphin yana taka muhimmiyar rawa wajen hana yaduwar nociceptive a matakin kashin baya.
Naloxone na iya jujjuya juzu'i (kusan 50%) tasirin hanawa na dermorphin akan nociceptive spinal reflex. Wannan na iya nufin cewa dermorphin yana hulɗa tare da mutane daban-daban na masu karɓar opioid na kashin baya don haifar da sakamako na analgesic [2].
Tasiri kan Tsarin Jijiya ta Tsakiya
Gudanar da intracerebroventricular na DM yana haifar da aikin antinociceptive na dogon lokaci [1] . Wannan yana nuna cewa dermorphin na iya haifar da tasirin analgesic ta hanyar aiki akan tsarin juyayi na tsakiya. Duk da haka, takamaiman aikin aikin dermorphin a cikin tsarin kulawa na tsakiya ba a fahimta ba tukuna.
A cikin gwaje-gwajen zomo, bayan allurar dermorphin ta cikin jijiya, halayen zomaye sun nuna karuwa mai yawa a lokacin zaman shiru da rashin motsi, da raguwar ayyukan son rai, amma ba shi da tasiri a kan tsari da mita na electroencephalogram na hippocampal [3] . Wannan yana nuna cewa dermorphin na iya yin tasiri a kan wasu halaye na musamman da yankunan tsarin jin tsoro.
3. Tasirin Gastrointestinal Tract
Dermorphin yana da tasiri akan haɓakar hanji a cikin berayen. Idan aka kwatanta da morphine, allurar intracerebroventricular na dermorphin yana hana haɓakar hanji kamar morphine, kuma aikinsa shine sau 143 na morphine [4] . Sakamakon adawa na naloxone akan dermorphin ba shi da tasiri fiye da haka akan morphine. Gudanar da intracerebroventricular naloxone quaternized naloxone zai iya ƙin tasirin intracerebroventricular dermorphin akan hanji, yayin da allurar intraperitoneal kawai ke tasiri a kashi 8mg/kg. Dermorphin da ake gudanarwa ta intraperitoneally ba shi da tasiri gaba ɗaya a matsakaicin matsakaicin tasiri (0.56 micrograms da bera). Ƙara yawan allurar intraperitoneal na dermorphin (daga 12 zuwa 6400 micrograms a kowace kilogiram) yana da tasiri mai hanawa akan haɓakar hanji wanda ke zaman kansa daga kashi, amma bai wuce 50% ba. Babban adadin naloxone kawai (30mg/kg, allurar intraperitoneal) zai iya ƙin tasirin wannan allurar ta cikin peritoneal. Wannan yana nuna cewa tasirin dermorphin akan hanji zai iya haɗawa da sassan tsakiya da na gefe.
4. Tasirin Tsoka
An yi nazarin aikin Dermorphin akan sashin giciye na tsokar ciki na kwadi ta mai rikodin injina [5] . Sakamakon binciken ya nuna cewa dermorphin (10 (-5) -10 (-8) M) zai iya toshe aikin acetylcholine, aiki maras lokaci, da ƙwayar tsoka wanda ya haifar da haɓakar wutar lantarki kai tsaye. Duk waɗannan illolin suna da wahalar juyewa. Idan an allurar dermorphin a cikin matsakaicin shiryawa yayin K (+) depolarization (KCl - 100mM) na tsoka, ba zai iya toshe ayyukan da ba a kai ba. Saboda haka, dermorphin yana da tasiri mai dogara da ƙarfin lantarki kuma yana iya yin aiki akan tashoshi na Ca (2+) masu dogara da wutar lantarki na ƙwayar ƙwayar tsoka.
5. Dangantaka Tsakanin Tsarin Halitta da Tsarin Aiki
An gudanar da siminti na inji akan dermorphin (Pattabiraman N, 1986). Binciken ya nuna cewa D-Ala2 a N-terminus da sauran L-Pro6 a C-terminus a cikin jerin dermorphin suna nuna yiwuwar kasancewar β-juyawa. Daga hangen nesa na sitiriyo, ana iya samun nau'i uku (II', III', da V') na β-juyawa a N-terminus na peptide, da nau'i biyu (I da III) na β-juyawa a C-terminus. In the molecular mechanics calculations, six folded conformations and one extended conformation were considered to evaluate the relative stability of dermorphin. Among them, three folded conformations have lower energy and have the following general characteristics: similar energy, three hydrogen bonds, a semi-rigid β-sheet fragment, and a favorable Tyr1-Tyr5 interaction. Kasancewar tsarin β-sheet na iya taka rawa a cikin zaɓin hulɗar tsakanin dermorphin da μ-receptor.
Menene aikace-aikacen Dermorphin?
An yi amfani da shi don Gudanar da Pain Pain: Wani binciken da aka bazu, binciken da aka gudanar a cikin 1985 ya nuna cewa Dermorphin da aka gudanar ta hanyar intrathecal ya fi tasiri fiye da placebo da kuma morphine mai mahimmanci a cikin ciwon ciwon ciwon baya [6, 7] . Wannan yana nuna cewa Dermorphin na iya samun babban tasiri wajen kawar da ciwon baya. Ga marasa lafiya na baya-bayan nan, kulawar jin zafi mai tasiri ba zai iya inganta jin dadin marasa lafiya kawai ba amma kuma ya taimaka wa marasa lafiya su dawo da komawa rayuwa ta al'ada.
Aikace-aikace a cikin Kulawa na Palliative: Yin la'akari da kyakkyawan sakamako na analgesic, Dermorphin kuma an ba da shawarar don amfani da shi a cikin kula da marasa lafiya na ci gaba [6, 7] . A cikin kulawar jin daɗin jin daɗi, kawar da radadin marasa lafiya shine manufa mai mahimmanci, kuma Dermorphin, tare da tasirin analgesic mai ƙarfi da ƙarancin haɗarin sakamako masu illa, yana ba da zaɓi mai yuwuwa don kawar da radadin marasa lafiya da suka ci gaba.
Inhibitory Effect on Spinal Pain: Studies have shown that Dermorphin can inhibit the transmission of nociception in the spinal cord. A cikin masu aikin sa kai masu lafiya, jiko na 0.16mg/kg na Dermorphin na iya zama mai mahimmanci kuma a ci gaba da haɓaka bakin kofa na nociceptive flexor reflex [8] . Hakanan an lura da irin wannan tasirin a cikin batutuwa masu cikakken rauni na kashin baya, yana nuna cewa Dermorphin ya fi yin aiki a matakin kashin baya don hana watsa jin zafi. Wannan sakamako mai hanawa akan ciwon kashin baya yana ba da sabon bege don kula da marasa lafiya da ke fama da cututtukan cututtuka na kashin baya.
A ƙarshe, Dermorphin shine peptide mai ƙarfi na opioid-kamar wanda zai iya ɗaure ga masu karɓa na μ-opioid, yana nuna sakamako mai mahimmanci na analgesic da kuma hana watsa siginar nociceptive a cikin kashin baya. Yana da aikace-aikacen da za a iya amfani da su a cikin kula da ciwo na baya-bayan nan, kula da jin dadi, da dai sauransu, yana kawo sababbin ra'ayoyin don maganin ciwo.
Game da Marubuci
Abubuwan da aka ambata a sama duk bincike ne, gyara su kuma Cocer Peptides ne suka haɗa su.
Mawallafin Jaridar Kimiyya
Giuliano Fontani mai bincike ne da ke da alaƙa da Jami'ar Siena, Italiya, yana mai da hankali kan ilimin kimiyyar ƙwaƙwalwa da ilimin lissafi. Ya yi nazarin tasirin dermorphin, peptide na halitta, akan hali da aikin lantarki na hippocampal a cikin zomaye, yana ba da gudummawa ga fahimtar aikin mai karɓar opioid. Har ila yau, aikinsa ya bincika dangantakar dake tsakanin ayyukan kwakwalwa da hali, tare da wallafe-wallafe a cikin mujallu kamar Life Sciences. An jera Giuliano Fontani a cikin ambaton ambaton [3].
▎ Abubuwan da suka dace
[1] Mizusawa K. Dermorphin [M]//2021:107-109.DOI:10.1016/b978-0-12-820649-2.00027-9.
[2] Sandrini G, Degli Uberti EC, Salvadori S, et al. Dermorphin yana hana kashin baya nociceptive flexion reflex a cikin mutane [J]. Binciken Kwakwalwa, 1986,371 (2): 364-367.DOI: 10.1016 / 0006-8993 (86) 90376-8.
[3] Fontani G, Vergnani L, Salvadori S, et al. Tasirin dermorphin akan hali da ayyukan lantarki na hippocampal a cikin zomaye[J]. Kimiyyar Rayuwa, 1993,52(3):323-328.DOI:10.1016/0024-3205(93)90224-q.
[4] Parolaro D, Sala M, Crema G, et al. Abubuwan tsakiya da na gefe na tasirin dermorphin akan motsin hanji na bera idan aka kwatanta da morphine[J]. Peptides, 1983,4 (1): 55-58.DOI: 10.1016/0196-9781 (83) 90165-1.
[5] Babskaia N E. Ayyukan dogaro da kai na opioid peptide dermorphin[J]. Biull Eksp Biol Med, 1992,114 (11): 502-504. https://pubmed.ncbi.nlm.nih.gov/1363279/.
[6] Hesselink JMK, Schatman M E. Sake gano tsoffin magunguna: lamarin da aka manta na dermorphin don jin zafi da jin zafi [J]. Journal of Pain Research, 2018,11:2991-2995.DOI:10.2147/JPR.S186082.
[7] Keppel Hesselink J, Schatman M. Journal of Pain Research, 2018,11:2991.DOI:10.2147/JPR.S186082.
[8] Pattabiraman N, Sorensen KR, Langridge R, et al. Nazarin injiniyoyin kwayoyin halitta na dermorphin [J]. Hanyoyin Sadarwar Bincike na Biochemical da Biophysical, 1986,140(1):342-349.DOI:10.1016/0006-291x(86)91096-x.
DUKKANIN LABARI DA BAYANIN KYAUTATAWA DA AKE BAYAR A WANNAN SHAFIN KAWAI DOMIN WATSA BAYANI NE DA MANUFOFIN ILIMI.
Kayayyakin da aka bayar akan wannan gidan yanar gizon an yi niyya ne kawai don binciken in vitro. Binciken in vitro (Latin: *a cikin gilashi*, ma'ana a cikin gilashin gilashi) ana gudanar da shi a wajen jikin mutum. Waɗannan samfuran ba magunguna ba ne, Hukumar Abinci da Magunguna ta Amurka (FDA) ba ta amince da su ba, kuma dole ne a yi amfani da su don hanawa, magani, ko warkar da duk wani yanayi na likita, cuta, ko cuta. Doka ta haramta shigar da waɗannan samfuran cikin jikin mutum ko dabba ta kowace hanya.